Synthesis and acetylcholinesterase inhibition of 5-desamino huperzine A derivatives

Bioorg Med Chem Lett. 2001 Oct 8;11(19):2627-30. doi: 10.1016/s0960-894x(01)00518-2.

Abstract

(E)- and (Z)-5-Desamino huperzine A derivatives have been synthesized using a new synthetic strategy towards the huperzine A skeleton. These derivatives showed AChE inhibition constants in the low micromolar range and thus display better activity than all previously synthesized C5 derivatives.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholinesterase / metabolism
  • Animals
  • Bridged-Ring Compounds / chemical synthesis*
  • Bridged-Ring Compounds / chemistry
  • Bridged-Ring Compounds / pharmacology
  • Cholinesterase Inhibitors / chemical synthesis*
  • Cholinesterase Inhibitors / chemistry
  • Cholinesterase Inhibitors / pharmacology
  • Heterocyclic Compounds, 3-Ring / chemical synthesis*
  • Heterocyclic Compounds, 3-Ring / chemistry
  • Heterocyclic Compounds, 3-Ring / pharmacology
  • Rats
  • Rats, Sprague-Dawley

Substances

  • 5-desamino huperzine A
  • Bridged-Ring Compounds
  • Cholinesterase Inhibitors
  • Heterocyclic Compounds, 3-Ring
  • Acetylcholinesterase